scholarly journals Interactions of primaquine and chloroquine with PEGylated phosphatidylcholine liposomes

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Andang Miatmoko ◽  
Ira Nurjannah ◽  
Nuril Fadilatul Nehru ◽  
Noorma Rosita ◽  
Esti Hendradi ◽  
...  
Keyword(s):  
Membrane Integrity ◽  
Bilayer Membrane ◽  
Head Group ◽  
Polar Head Group ◽  
X Ray Diffraction ◽  
Liposomal Membrane ◽  
Phosphatidylcholine Liposomes ◽  
Calcein Release ◽  
Crystallinity Changes ◽  
Film Method

AbstractThis study aimed to analyze the interaction of primaquine (PQ), chloroquine (CQ), and liposomes to support the design of optimal liposomal delivery for hepatic stage malaria infectious disease. The liposomes were composed of hydrogenated soybean phosphatidylcholine, cholesterol, and distearoyl-sn-glycero-3-phosphoethanolamine-N-(methoxy[polyethyleneglycol]-2000), prepared by thin film method, then evaluated for physicochemical and spectrospic characteristics. The calcein release was further evaluated to determine the effect of drug co-loading on liposomal membrane integrity. The results showed that loading PQ and CQ into liposomes produced changes in the infrared spectra of the diester phosphate and carbonyl ester located in the polar part of the phospholipid, in addition to the alkyl group (CH2) in the nonpolar portion. Moreover, the thermogram revealed the loss of the endothermic peak of liposomes dually loaded with PQ and CQ at 186.6 °C, which is identical to that of the phospholipid. However, no crystallinity changes were detected through powder X-ray diffraction analysis. Moreover, PQ, with either single or dual loading, produced the higher calcein release profiles from the liposomes than that of CQ. The dual loading of PQ and CQ tends to interact with the polar head group of the phosphatidylcholine bilayer membrane resulted in an increase in water permeability of the liposomes.

scholarly journals Molecular dynamics simulations and experimental studies reveal differential permeability of withaferin-A and withanone across the model cell membrane

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Renu Wadhwa ◽  
Neetu Singh Yadav ◽  
Shashank P. Katiyar ◽  
Tomoko Yaguchi ◽  
Chohee Lee ◽  
...  
Keyword(s):  
Molecular Dynamics ◽  
Cell Membrane ◽  
Molecular Dynamics Simulations ◽  
Experimental Studies ◽  
Bilayer Membrane ◽  
Withaferin A ◽  
Head Group ◽  
Polar Head Group ◽  
Natural Drugs ◽  
Dynamics Simulations

AbstractPoor bioavailability due to the inability to cross the cell membrane is one of the major reasons for the failure of a drug in clinical trials. We have used molecular dynamics simulations to predict the membrane permeability of natural drugs—withanolides (withaferin-A and withanone) that have similar structures but remarkably differ in their cytotoxicity. We found that whereas withaferin-A, could proficiently transverse through the model membrane, withanone showed weak permeability. The free energy profiles for the interaction of withanolides with the model bilayer membrane revealed that whereas the polar head group of the membrane caused high resistance for the passage of withanone, the interior of the membrane behaves similarly for both withanolides. The solvation analysis further revealed that the high solvation of terminal O5 oxygen of withaferin-A was the major driving force for its high permeability; it interacted with the phosphate group of the membrane that led to its smooth passage across the bilayer. The computational predictions were tested by raising and recruiting unique antibodies that react to withaferin-A and withanone. The time-lapsed analyses of control and treated cells demonstrated higher permeation of withaferin-A as compared to withanone. The concurrence between the computation and experimental results thus re-emphasised the use of computational methods for predicting permeability and hence bioavailability of natural drug compounds in the drug development process.

Comparative Analysis of Crystallinity Changes in Cellulose I Polymers Using ATR-FTIR, X-ray Diffraction, and Carbohydrate-Binding Module Probes

2011 ◽  
Vol 12 (11) ◽  
pp. 4121-4126 ◽  
Author(s):  
Alenka Kljun ◽  
Thomas A. S. Benians ◽  
Florence Goubet ◽  
Frank Meulewaeter ◽  
J. Paul Knox ◽  
...  
Keyword(s):  
Comparative Analysis ◽  
Carbohydrate Binding ◽  
Carbohydrate Binding Module ◽  
X Ray Diffraction ◽  
Cellulose I ◽  
X Ray ◽  
Crystallinity Changes

The effect of polar head group of dodecyl surfactants on the growth of wheat and cucumber

Chemosphere ◽  
2020 ◽  
Vol 254 ◽  
pp. 126918
Author(s):  
Aleksandar Tot ◽  
Ivana Maksimović ◽  
Marina Putnik-Delić ◽  
Milena Daničić ◽  
Slobodan Gadžurić ◽  
...  
Keyword(s):  
Head Group ◽  
Polar Head Group ◽  
Polar Head

Hemolytic Activity of Aminoethyl-dodecanoates

1998 ◽  
Vol 53 (1-2) ◽  
pp. 101-106 ◽  
Author(s):  
H. Kleszczyńska ◽  
J. Łuczyński ◽  
S. Witek ◽  
S. Przestalski
Keyword(s):  
Plasma Membrane ◽  
Membrane Fluidity ◽  
Erythrocyte Membrane ◽  
Hemolytic Activity ◽  
Protonated Form ◽  
Maximum Activity ◽  
Head Group ◽  
Dodecanoic Acid ◽  
Polar Head Group ◽  
Erythrocyte Membrane Fluidity

Abstract The effect of new lysosomotropic compounds on red blood cell hemolysis and erythrocyte membrane fluidity has been investigated. In earlier studies it was shown that the compounds inhibit the growth of yeast and plasma membrane H+-ATPase activity. The study was per­ formed with eight aminoethyl esters of lauric acid variously substituted at nitrogen atom. Esters of dodecanoic acid were chosen for study because at that chain length dimethylaminoethyl esters showed maximum activity. The hemolytic activity of the substances studied exhib­its diversified activity in their interaction with the erythrocyte membrane: they differ in hemolytic activity and affect membrane fluidity differently. Erythrocyte membrane fluidity changes under the effect of those compounds which possess highest hemolytic activity. The hemolytic activity of the aminoesters investigated was found to follow a sequence that de­pended on basicity (i.e. ability of the protonated form formation) of the compound and its polar head group size. The most active are the compounds that possess not more than four carbon atoms substituted at nitrogen and highest pKa value.

Glycosylinositol phosphoceramide-specific phospholipase D activity catalyzes transphosphatidylation

2019 ◽  
Vol 166 (5) ◽  
pp. 441-448 ◽  
Author(s):  
Rumana Yesmin Hasi ◽  
Makoto Miyagi ◽  
Katsuya Morito ◽  
Toshiki Ishikawa ◽  
Maki Kawai-Yamada ◽  
...  
Keyword(s):  
Chain Length ◽  
Phospholipase D ◽  
Secondary Alcohol ◽  
Primary Alcohol ◽  
Tertiary Alcohol ◽  
Head Group ◽  
Polar Head Group ◽  
Polar Head ◽  
A Chain ◽  
Sugar Chains

Abstract Glycosylinositol phosphoceramide (GIPC) is the most abundant sphingolipid in plants and fungi. Recently, we detected GIPC-specific phospholipase D (GIPC-PLD) activity in plants. Here, we found that GIPC-PLD activity in young cabbage leaves catalyzes transphosphatidylation. The available alcohol for this reaction is a primary alcohol with a chain length below C4. Neither secondary alcohol, tertiary alcohol, choline, serine nor glycerol serves as an acceptor for transphosphatidylation of GIPC-PLD. We also found that cabbage GIPC-PLD prefers GIPC containing two sugars. Neither inositol phosphoceramide, mannosylinositol phosphoceramide nor GIPC with three sugar chains served as substrate. GIPC-PLD will become a useful catalyst for modification of polar head group of sphingophospholipid.

Ion movements in membrane vesicles: a new fluorescence method and application to smooth muscle

1985 ◽  
Vol 248 (3) ◽  
pp. C372-C378 ◽  
Author(s):  
A. K. Grover ◽  
A. P. Singh ◽  
P. K. Rangachari ◽  
P. Nicholls
Keyword(s):  
Membrane Potential ◽  
Membrane Permeability ◽  
Membrane Vesicles ◽  
Liposomal Membrane ◽  
Phosphatidylcholine Liposomes ◽  
Permeability Characteristics ◽  
Cation Permeability ◽  
Ion Movements ◽  
Rate Of Dissipation ◽  
Very High

A method is described for studying ion permeabilities of membrane vesicles based on the principle that when membrane permeability to H+ is very high, the H+ movement is determined by the membrane potential generated by the H+ movement. The rate of H+ movement under these conditions thus gives a measure of the rate of dissipation of this membrane potential by comovement of anions or countermovement of cations present. Thus, by studying the H+ efflux using an impermeant cation and different anions, the membrane permeability to the anions can be assessed. Similarly, the use of an impermeant anion allows the study of the permeation of various cations. H+ movement was followed across the membranes by monitoring a change in the fluorescence intensity of the pH-sensitive dye pyranine trapped inside the membranes. This method when tested using phosphatidylcholine liposomes yielded the expected results, i.e., permeability of the liposomal membrane was: Cl- greater than SO2-4 and K+ greater than Na+. A plasma membrane-enriched fraction loaded with pyranine was isolated from estrogen-dominant rat myometrium. The anion permeability characteristics of this membrane were studied using tetramethylammonium (TMA+) as the poorly permeant cation, and the cation permeability was studied using L-glutamate- as the poorly permeant anion. The anion permeabilities were D-glutamate- less than L-glutamate- less than glutarate2- less than Cl- less than or equal to SO2-4, and the cation permeabilities were TMA+ less than K+ less than Na+. It is hypothesized that the observed anomalously higher Na+ and SO2-4 movements may involve special mechanisms.

Sign in / Sign up

Export Citation Format

Share Document